Action and mechanism

The main pharmacological effect of oxerutins is to reduce water filtration rates and microvascular permeability to proteins. Through their action on the vascular endothelium, stabilizing the endothelial membrane and consequently reducing capillary permeability, oxerutins clinically address edematous infiltration, pain, trophic disorders, and the various pathological manifestations that characterize chronic venous insufficiency.

Pharmacokinetics

The pharmacokinetics of oxerutins have been studied in mice, rats, dogs, rhesus monkeys, and humans. The progressive substitution of hydroxyl groups in the original rutin molecule with hydroxyethyl groups results in increased water solubility, greater resistance of the molecule to bacterial degradation in the intestine, and decreased protein binding. This weak and reversible protein binding of oxerutins is approximately 30%. The detection of oxerutin glycosides and their corresponding glucuronides in urine and bile (14–20% of an oral dose administered to rats) demonstrates that the compound is absorbed. There is a high hepatic first-pass effect and enterohepatic circulation.
Elimination occurs primarily through the biliary tract (approximately 65% of the molecule eliminated) and the urinary tract, and this excretion is virtually complete within 24 to 48 hours. Oxerutins do not cross the blood-brain barrier.
After oral or intravenous administration, oxerutins cross the placenta minimally, with only traces found in rat or mouse fetuses. Similarly, only traces of oxerutins have been found in the milk of lactating rats.
In humans, following oral administration of 14C-oxerutins, peak plasma concentrations occur between 1 and 9 hours, with detectable levels observed up to 120 hours after administration. The concentration decline occurs biexponentially. 3–6% of the administered radioactivity is excreted in urine within 48 hours. The apparent elimination half-life varies from 10 to 25 hours but is relatively constant for the same individual. Biliary elimination of oxerutins, as well as the formation of glucuronide metabolites, has been confirmed in humans.

Indications

- [VENOUS INSUFFICIENCY] mild. Treatment in adults of symptoms associated with mild venous insufficiency of the lower extremities, such as pain, heaviness, tightness, tingling, and itching in legs with varicose veins or swollen legs.

Posology

- Adults, oral: Initial dose: 1 sachet/day. Symptom relief usually occurs within the first 2 weeks.
If you do not feel relief after 2 weeks or your symptoms worsen, you should consult your doctor and continue treatment for up to 2-3 months.

Rules for correct administration

Dissolve the contents of the sachet in 1 glass of water and drink immediately.

Contraindications

- Known hypersensitivity to any of the components.

Precautions

- Special clinical monitoring should be performed in patients with [PEPTIC ULCER], severe [HEMORRHAGE] or [THROMBOPENIA].

Pregnancy

There is no evidence that it may have any harmful effects on the fetus or newborn during pregnancy. However, women planning a pregnancy or in the first trimester of pregnancy should be advised to take this medication only under medical prescription.

Lactation

No specific data are available in humans; it is advisable to discontinue treatment during breastfeeding.

Adverse reactions

The following adverse reactions have been reported, mainly associated with the use of the oral form, with a frequency of rare (0.01-0.1%) or very rare (<0.01%):

- Digestive: Rare: [FLATULENCE], [DIARRHEA], [GASTRALGIA], gastric discomfort and [DYSPEPSIA].

- Cardiovascular: Very rare: [BLUSHING]

- Neurological/psychological: Very rare: [HEADACHE] and [DIZZINESS].

- Allergic/dermatological: Rare: [EXANTHEMATOUS RASHES], [PRURITUS] and [URTICARIA]. Very rare: [ANAPHYLAXIS], anaphylactoid reactions and [HYPERSENSITIVITY REACTIONS]. Skin reactions, the main adverse reactions reported with topical use, usually disappear when treatment is discontinued.

- General: Very rare: [ASTHENIA].